The enhanced in vivo activity of the combination of a MEK and a PI3K inhibitor correlates with [18F]-FLT PET in human colorectal cancer xenograft tumour-bearing mice.

PubWeight™: 0.81‹?›

🔗 View Article (PMC 3858267)

Published in PLoS One on December 10, 2013

Authors

Emma J Haagensen1, Huw D Thomas, Ian Wilson, Suzannah J Harnor, Sara L Payne, Tommy Rennison, Kate M Smith, Ross J Maxwell, David R Newell

Author Affiliations

1: Newcastle Cancer Centre, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Newcastle University, Framlington Place, Newcastle-upon-Tyne, United Kingdom.

Articles cited by this

AKT/PKB signaling: navigating downstream. Cell (2007) 31.26

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers. Nat Med (2008) 14.47

Protein kinase B/Akt-mediated phosphorylation promotes nuclear exclusion of the winged helix transcription factor FKHR1. Proc Natl Acad Sci U S A (1999) 7.70

FOXO transcription factors at the interface between longevity and tumor suppression. Oncogene (2005) 7.50

Guidelines for the welfare and use of animals in cancer research. Br J Cancer (2010) 6.97

Multiple Ras-dependent phosphorylation pathways regulate Myc protein stability. Genes Dev (2000) 6.54

ERK promotes tumorigenesis by inhibiting FOXO3a via MDM2-mediated degradation. Nat Cell Biol (2008) 5.19

Tumor-promoting phorbol esters and activated Ras inactivate the tuberous sclerosis tumor suppressor complex via p90 ribosomal S6 kinase. Proc Natl Acad Sci U S A (2004) 5.16

Imaging proliferation in vivo with [F-18]FLT and positron emission tomography. Nat Med (1998) 5.14

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . J Med Chem (2008) 4.49

The BAD protein integrates survival signaling by EGFR/MAPK and PI3K/Akt kinase pathways in PTEN-deficient tumor cells. Cancer Cell (2005) 4.48

Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition. Proc Natl Acad Sci U S A (2009) 4.02

Phosphorylation and inactivation of BAD by mitochondria-anchored protein kinase A. Mol Cell (1999) 3.46

Predictive biomarkers of sensitivity to the phosphatidylinositol 3' kinase inhibitor GDC-0941 in breast cancer preclinical models. Clin Cancer Res (2010) 3.20

p70S6 kinase signals cell survival as well as growth, inactivating the pro-apoptotic molecule BAD. Proc Natl Acad Sci U S A (2001) 3.11

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer. Proc Natl Acad Sci U S A (2009) 2.77

Regulation of human thymidine kinase during the cell cycle. J Biol Chem (1988) 2.67

Validation of FLT uptake as a measure of thymidine kinase-1 activity in A549 carcinoma cells. J Nucl Med (2002) 2.54

3'-deoxy-3'-[18F]fluorothymidine as a new marker for monitoring tumor response to antiproliferative therapy in vivo with positron emission tomography. Cancer Res (2003) 2.46

Imaging early changes in proliferation at 1 week post chemotherapy: a pilot study in breast cancer patients with 3'-deoxy-3'-[18F]fluorothymidine positron emission tomography. Eur J Nucl Med Mol Imaging (2007) 2.35

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett (2008) 2.28

A phase II study of PD-0325901, an oral MEK inhibitor, in previously treated patients with advanced non-small cell lung cancer. Clin Cancer Res (2010) 1.95

Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration. Cancer Chemother Pharmacol (2006) 1.71

18F-FLT PET during radiotherapy or chemoradiotherapy in head and neck squamous cell carcinoma is an early predictor of outcome. J Nucl Med (2013) 1.69

Activation of PI3K/Akt and MAPK pathways regulates Myc-mediated transcription by phosphorylating and promoting the degradation of Mad1. Proc Natl Acad Sci U S A (2008) 1.69

p90(RSK) blocks bad-mediated cell death via a protein kinase C-dependent pathway. J Biol Chem (1999) 1.67

Usefulness of 3'-[F-18]fluoro-3'-deoxythymidine with positron emission tomography in predicting breast cancer response to therapy. Mol Imaging Biol (2006) 1.60

Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res (2011) 1.56

Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors. Cancer Res (2010) 1.49

3-deoxy-3-[(18)F]fluorothymidine-positron emission tomography for noninvasive assessment of proliferation in pulmonary nodules. Cancer Res (2002) 1.46

Correlation between Ki-67 immunohistochemistry and 18F-fluorothymidine uptake in patients with cancer: A systematic review and meta-analysis. Eur J Cancer (2012) 1.41

[(18)F]FLT-PET imaging does not always "light up" proliferating tumor cells. Clin Cancer Res (2011) 1.35

In vivo activity of combined PI3K/mTOR and MEK inhibition in a Kras(G12D);Pten deletion mouse model of ovarian cancer. Mol Cancer Ther (2011) 1.23

The role of human nucleoside transporters in uptake of 3'-deoxy-3'-fluorothymidine. Mol Pharmacol (2008) 1.14

Limits of [18F]-FLT PET as a biomarker of proliferation in oncology. PLoS One (2013) 1.12

Post-translational regulation of the ERK phosphatase DUSP6/MKP3 by the mTOR pathway. Oncogene (2008) 1.09

MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo. Mol Cancer Ther (2010) 1.08

FDG-PET is a good biomarker of both early response and acquired resistance in BRAFV600 mutant melanomas treated with vemurafenib and the MEK inhibitor GDC-0973. EJNMMI Res (2012) 1.08

GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo. Clin Cancer Res (2012) 1.07

Gastric cancer growth control by BEZ235 in vivo does not correlate with PI3K/mTOR target inhibition but with [18F]FLT uptake. Clin Cancer Res (2011) 1.06

3'-deoxy-3'-[18F]fluorothymidine positron emission tomography is a sensitive method for imaging the response of BRAF-dependent tumors to MEK inhibition. Cancer Res (2007) 1.04

The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. Br J Cancer (2012) 1.03

Molecular imaging of proliferation in vivo: positron emission tomography with [18F]fluorothymidine. Methods (2009) 1.01

Detection and grading of soft tissue sarcomas of the extremities with (18)F-3'-fluoro-3'-deoxy-L-thymidine. Clin Cancer Res (2004) 0.99

Glucose metabolism measured by [¹⁸F]fluorodeoxyglucose positron emission tomography is independent of PTEN/AKT status in human colon carcinoma cells. Transl Oncol (2011) 0.98

Noninvasive imaging of cell proliferation following mitogenic extracellular kinase inhibition by PD0325901. Mol Cancer Ther (2008) 0.96

Inhibition of PI3K and MEK: it is all about combinations and biomarkers. Clin Cancer Res (2009) 0.96

Comparison of [18F]-tracers in various experimental tumor models by PET imaging and identification of an early response biomarker for the novel microtubule stabilizer patupilone. Mol Imaging Biol (2009) 0.91

ZSTK474, a PI3K inhibitor, suppresses proliferation and sensitizes human pancreatic adenocarcinoma cells to gemcitabine. Oncol Rep (2011) 0.88

3D tumour spheroids as a model to assess the suitability of [18F]FDG-PET as an early indicator of response to PI3K inhibition. Nucl Med Biol (2012) 0.87

PI3K pathway inhibitors: better not left alone. Curr Pharm Des (2013) 0.87

Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human. Xenobiotica (2011) 0.84

Conventional and novel PET tracers for imaging in oncology in the era of molecular therapy. Cancer Treat Rev (2007) 0.83

[18F]-FLT positron emission tomography can be used to image the response of sensitive tumors to PI3-kinase inhibition with the novel agent GDC-0941. Mol Cancer Ther (2013) 0.81

(18)F-FLT-PET for Response Evaluation of MEK Inhibitor Selumetinib (AZD6244, ARRY-142886) in Patients with Solid Tumors. World J Nucl Med (2012) 0.77

Articles by these authors

Specific killing of BRCA2-deficient tumours with inhibitors of poly(ADP-ribose) polymerase. Nature (2005) 19.13

Activation of the mucosal immune system in irritable bowel syndrome. Gastroenterology (2002) 5.50

Defining professionalism in medical education: a systematic review. Med Teach (2013) 3.07

Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361. J Natl Cancer Inst (2004) 2.72

Nitric oxide, stomatal closure, and abiotic stress. J Exp Bot (2008) 2.55

Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res (2006) 2.45

Combretastatin A4 phosphate has tumor antivascular activity in rat and man as demonstrated by dynamic magnetic resonance imaging. J Clin Oncol (2003) 2.35

Compromised CDK1 activity sensitizes BRCA-proficient cancers to PARP inhibition. Nat Med (2011) 2.35

Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther (2007) 1.85

Minimally invasive pharmacokinetic and pharmacodynamic technologies in hypothesis-testing clinical trials of innovative therapies. J Natl Cancer Inst (2006) 1.83

Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2. J Natl Cancer Inst (2010) 1.74

Pharmacokinetic investigation of imatinib using accelerator mass spectrometry in patients with chronic myeloid leukemia. Clin Cancer Res (2007) 1.66

The value of hyperbilirubinaemia in the diagnosis of acute appendicitis. Ann R Coll Surg Engl (2011) 1.62

Teaching professionalism in medical education: a Best Evidence Medical Education (BEME) systematic review. BEME Guide No. 25. Med Teach (2013) 1.50

Mutations in the SPG7 gene cause chronic progressive external ophthalmoplegia through disordered mitochondrial DNA maintenance. Brain (2014) 1.49

Transient treatment with CDK inhibitors eliminates proliferative potential even when their abilities to evoke apoptosis and DNA damage are blocked. Cell Cycle (2008) 1.47

Long-term effects of childhood abuse on the quality of life and health of older people: results from the Depression and Early Prevention of Suicide in General Practice Project. J Am Geriatr Soc (2007) 1.46

Directed evolution of N-acetylneuraminic acid aldolase to catalyze enantiomeric aldol reactions. Bioorg Med Chem (2003) 1.44

Psychiatric comorbidity in general practice. Aust Fam Physician (2004) 1.39

Temozolomide pharmacodynamics in patients with metastatic melanoma: dna damage and activity of repair enzymes O6-alkylguanine alkyltransferase and poly(ADP-ribose) polymerase-1. Clin Cancer Res (2005) 1.37

Intravital imaging of tumour vascular networks using multi-photon fluorescence microscopy. Adv Drug Deliv Rev (2005) 1.31

Nitric oxide evolution and perception. J Exp Bot (2007) 1.31

6-thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance. Cancer Res (2010) 1.29

Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor. Nat Struct Biol (2002) 1.27

Novel poly(ADP-ribose) polymerase-1 inhibitor, AG14361, restores sensitivity to temozolomide in mismatch repair-deficient cells. Clin Cancer Res (2004) 1.27

Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res (2009) 1.25

Asthma and depression: a pragmatic review of the literature and recommendations for future research. Clin Pract Epidemiol Ment Health (2005) 1.24

Case report of recurrent acute appendicitis in a residual tip. Cases J (2010) 1.13

Spatial and temporal properties of gestures in North American English /r/. Lang Speech (2010) 1.11

Systems toxicology: integrated genomic, proteomic and metabonomic analysis of methapyrilene induced hepatotoxicity in the rat. J Proteome Res (2006) 1.08

Identification of potent nontoxic poly(ADP-Ribose) polymerase-1 inhibitors: chemopotentiation and pharmacological studies. Clin Cancer Res (2003) 1.08

UPLC-MS-based analysis of human plasma for metabonomics using solvent precipitation or solid phase extraction. J Proteome Res (2009) 1.05

Vasoactivity of AG014699, a clinically active small molecule inhibitor of poly(ADP-ribose) polymerase: a contributory factor to chemopotentiation in vivo? Clin Cancer Res (2009) 1.04

'Part of the team': professional identity and social exclusivity in medical students. Med Educ (2011) 1.03

Preclinical evaluation of a novel ATM inhibitor, KU59403, in vitro and in vivo in p53 functional and dysfunctional models of human cancer. Mol Cancer Ther (2013) 1.02

Language-specific articulatory settings: evidence from inter-utterance rest position. Phonetica (2005) 1.02

Metabonomic investigation of liver profiles of nonpolar metabolites obtained from alcohol-dosed rats and mice using high mass accuracy MSn analysis. J Proteome Res (2010) 1.00

Poly(ADP-ribose) polymerase-1 (PARP-1) pharmacogenetics, activity and expression analysis in cancer patients and healthy volunteers. Biochem J (2011) 0.99

Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinase 2. Org Biomol Chem (2007) 0.98

Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J Med Chem (2003) 0.98

Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure. J Med Chem (2002) 0.98

Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Mol Cancer Ther (2012) 0.97

Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther (2005) 0.97

Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. J Med Chem (2006) 0.96

Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer. PLoS One (2012) 0.96

Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination. Cancer Chemother Pharmacol (2011) 0.96

Patterning of the vertebrate ventral spinal cord. Int J Dev Biol (2002) 0.95

Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency. J Med Chem (2011) 0.95

The clinically active PARP inhibitor AG014699 ameliorates cardiotoxicity but does not enhance the efficacy of doxorubicin, despite improving tumor perfusion and radiation response in mice. Mol Cancer Ther (2011) 0.94

SlTPR1, a tomato tetratricopeptide repeat protein, interacts with the ethylene receptors NR and LeETR1, modulating ethylene and auxin responses and development. J Exp Bot (2008) 0.93

Non-specific binding of [18F]FDG to calcifications in atherosclerotic plaques: experimental study of mouse and human arteries. Eur J Nucl Med Mol Imaging (2006) 0.93

Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models. Mol Cancer Ther (2011) 0.93

A proteomic analysis of oligo(dT)-bound mRNP containing oxidative stress-induced Arabidopsis thaliana RNA-binding proteins ATGRP7 and ATGRP8. Mol Biol Rep (2009) 0.93

Toxoflavins and deazaflavins as the first reported selective small molecule inhibitors of tyrosyl-DNA phosphodiesterase II. J Med Chem (2013) 0.92

N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. J Med Chem (2004) 0.92

2-[11C]thymidine positron emission tomography as an indicator of thymidylate synthase inhibition in patients treated with AG337. J Natl Cancer Inst (2003) 0.91

The effect of commercial coaching on selection test performance. Med Teach (2012) 0.91

Estimation of apparent tumor vascular permeability from multiphoton fluorescence microscopic images of P22 rat sarcomas in vivo. Microcirculation (2008) 0.91

Uptake of inflammatory cell marker [11C]PK11195 into mouse atherosclerotic plaques. Eur J Nucl Med Mol Imaging (2008) 0.90

Pharmacokinetics of [¹⁸F]flutemetamol in wild-type rodents and its binding to beta amyloid deposits in a mouse model of Alzheimer's disease. Eur J Nucl Med Mol Imaging (2012) 0.90

Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. J Med Chem (2002) 0.90

Techniques for field application of lingual ultrasound imaging. Clin Linguist Phon (2005) 0.89

Effect of cell cycle inhibition on Cisplatin-induced cytotoxicity. J Pharmacol Exp Ther (2004) 0.89

Psychological comorbidity and complexity of gastrointestinal symptoms in clinically diagnosed irritable bowel syndrome patients. J Gastroenterol Hepatol (2007) 0.88

A randomized placebo-controlled trial of pre-treatment and short- or long-term maintenance therapy with amiodarone supporting DC cardioversion for persistent atrial fibrillation. Eur Heart J (2004) 0.88

Maintaining empathy in medical school: it is possible. Med Teach (2013) 0.88

Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo. Biochem Pharmacol (2012) 0.87

Imagining alternative professional identities: reconfiguring professional boundaries between nursing students and medical students. Acad Med (2015) 0.87

Validation of the fluorinated 2-nitroimidazole SR-4554 as a noninvasive hypoxia marker detected by magnetic resonance spectroscopy. Clin Cancer Res (2002) 0.87

No evidence of an association between mitochondrial DNA variants and osteoarthritis in 7393 cases and 5122 controls. Ann Rheum Dis (2012) 0.86

Clinical guidance on the use of antidepressant medications in children and adolescents. Aust Fam Physician (2005) 0.86

Non-invasive imaging of combretastatin activity in two tumor models: Association with invasive estimates. Acta Oncol (2010) 0.85

The community paediatrician - A vanishing breed? Paediatr Child Health (2002) 0.85

Medical education and moral segmentation in medical students. Med Educ (2013) 0.85

Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase. J Med Chem (2004) 0.85

Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction. Bioorg Med Chem Lett (2005) 0.85

Metabolic effects of a high-fat diet post-weaning after low maternal dietary folate during pregnancy and lactation. Mol Nutr Food Res (2014) 0.85

HPLC-MS/MS methods for the quantitative analysis of ophthalmic acid in rodent plasma and hepatic cell line culture medium. J Pharm Biomed Anal (2010) 0.84

Diclofenac metabolism in the mouse: novel in vivo metabolites identified by high performance liquid chromatography coupled to linear ion trap mass spectrometry. Xenobiotica (2011) 0.84

A GC-MS metabolic profiling study of plasma samples from mice on low- and high-fat diets. J Chromatogr B Analyt Technol Biomed Life Sci (2011) 0.84

Nitric oxide synthase inhibition enhances the tumor vascular-damaging effects of combretastatin a-4 3-o-phosphate at clinically relevant doses. Clin Cancer Res (2009) 0.84

Risk assessment and mitigation strategies for reactive metabolites in drug discovery and development. Chem Biol Interact (2010) 0.83

Side population in human non-muscle invasive bladder cancer enriches for cancer stem cells that are maintained by MAPK signalling. PLoS One (2012) 0.83

Radiological management of superior vena caval stent migration and infection. Cardiovasc Intervent Radiol (2005) 0.83

Measurement of extravascular lung water following human brain death: implications for lung donor assessment and transplantation. Eur J Cardiothorac Surg (2012) 0.83

MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones. Bioorg Med Chem Lett (2011) 0.83

Synthesis and biological evaluation of 5-substituted O4-alkylpyrimidines as CDK2 inhibitors. Org Biomol Chem (2010) 0.83

Searching for cyclin-dependent kinase inhibitors using a new variant of the cope elimination. J Am Chem Soc (2006) 0.83

In vitro approach to assess the potential for risk of idiosyncratic adverse reactions caused by candidate drugs. Chem Res Toxicol (2012) 0.83

Regioselective sulfamoylation at low temperature enables concise syntheses of putative small molecule inhibitors of sulfatases. Org Biomol Chem (2015) 0.83

4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2. Bioorg Med Chem Lett (2003) 0.83

Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase. J Med Chem (2007) 0.83